JPWO2022076285A5 - - Google Patents
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- Publication number
- JPWO2022076285A5 JPWO2022076285A5 JP2023520423A JP2023520423A JPWO2022076285A5 JP WO2022076285 A5 JPWO2022076285 A5 JP WO2022076285A5 JP 2023520423 A JP2023520423 A JP 2023520423A JP 2023520423 A JP2023520423 A JP 2023520423A JP WO2022076285 A5 JPWO2022076285 A5 JP WO2022076285A5
- Authority
- JP
- Japan
- Prior art keywords
- compound
- independently
- occurrence
- alkyl
- cycloalkyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 150000001875 compounds Chemical class 0.000 claims 56
- 125000000217 alkyl group Chemical group 0.000 claims 23
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 239000008194 pharmaceutical composition Substances 0.000 claims 15
- 125000003118 aryl group Chemical group 0.000 claims 12
- 125000001072 heteroaryl group Chemical group 0.000 claims 11
- 125000000623 heterocyclic group Chemical group 0.000 claims 8
- 229910052736 halogen Inorganic materials 0.000 claims 6
- 150000002367 halogens Chemical class 0.000 claims 6
- -1 cycloheteroalkyl Chemical group 0.000 claims 5
- 208000020832 chronic kidney disease Diseases 0.000 claims 4
- 125000004404 heteroalkyl group Chemical group 0.000 claims 4
- 230000002757 inflammatory effect Effects 0.000 claims 4
- 229910003827 NRaRb Inorganic materials 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 241000894007 species Species 0.000 claims 3
- 208000024827 Alzheimer disease Diseases 0.000 claims 2
- 208000023275 Autoimmune disease Diseases 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 201000004681 Psoriasis Diseases 0.000 claims 2
- 201000002661 Spondylitis Diseases 0.000 claims 2
- 206010052779 Transplant rejections Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 125000002877 alkyl aryl group Chemical group 0.000 claims 2
- 230000000903 blocking effect Effects 0.000 claims 2
- 229910052794 bromium Inorganic materials 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 208000015114 central nervous system disease Diseases 0.000 claims 2
- 208000022831 chronic renal failure syndrome Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 229910052731 fluorine Inorganic materials 0.000 claims 2
- 208000026278 immune system disease Diseases 0.000 claims 2
- 208000027866 inflammatory disease Diseases 0.000 claims 2
- 208000017169 kidney disease Diseases 0.000 claims 2
- 208000030159 metabolic disease Diseases 0.000 claims 2
- 201000006417 multiple sclerosis Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 208000028169 periodontal disease Diseases 0.000 claims 2
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 201000000596 systemic lupus erythematosus Diseases 0.000 claims 2
- 125000000876 trifluoromethoxy group Chemical group FC(F)(F)O* 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000001960 7 membered carbocyclic group Chemical group 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010009900 Colitis ulcerative Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 206010018367 Glomerulonephritis chronic Diseases 0.000 claims 1
- 208000022559 Inflammatory bowel disease Diseases 0.000 claims 1
- 208000032382 Ischaemic stroke Diseases 0.000 claims 1
- 108010027296 Kv1.3 Potassium Channel Proteins 0.000 claims 1
- 102000018706 Kv1.3 Potassium Channel Human genes 0.000 claims 1
- 201000006704 Ulcerative Colitis Diseases 0.000 claims 1
- 150000001350 alkyl halides Chemical class 0.000 claims 1
- 206010003246 arthritis Diseases 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 125000002393 azetidinyl group Chemical group 0.000 claims 1
- 125000001995 cyclobutyl group Chemical group [H]C1([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001786 isothiazolyl group Chemical group 0.000 claims 1
- 125000000842 isoxazolyl group Chemical group 0.000 claims 1
- 201000008383 nephritis Diseases 0.000 claims 1
- 201000001119 neuropathy Diseases 0.000 claims 1
- 230000007823 neuropathy Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 125000003566 oxetanyl group Chemical group 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 208000033808 peripheral neuropathy Diseases 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003226 pyrazolyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000001424 substituent group Chemical group 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063088171P | 2020-10-06 | 2020-10-06 | |
| US63/088,171 | 2020-10-06 | ||
| PCT/US2021/053320 WO2022076285A1 (en) | 2020-10-06 | 2021-10-04 | LACTAM COMPOUNDS AS Kv1.3 POTASSIUM SHAKER CHANNEL BLOCKERS |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023544404A JP2023544404A (ja) | 2023-10-23 |
| JPWO2022076285A5 true JPWO2022076285A5 (https=) | 2024-10-16 |
| JP2023544404A5 JP2023544404A5 (https=) | 2024-10-16 |
Family
ID=81126843
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023520423A Pending JP2023544404A (ja) | 2020-10-06 | 2021-10-04 | Ｋｖ１．３カリウムＳＨＡＫＥＲチャネル遮断剤としてのラクタム化合物 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230373952A1 (https=) |
| EP (1) | EP4225285A4 (https=) |
| JP (1) | JP2023544404A (https=) |
| KR (1) | KR20230082041A (https=) |
| CN (1) | CN116782894A (https=) |
| AU (1) | AU2021358700A1 (https=) |
| BR (1) | BR112023005387A2 (https=) |
| CA (1) | CA3193554A1 (https=) |
| IL (1) | IL301627A (https=) |
| MX (1) | MX2023003841A (https=) |
| WO (1) | WO2022076285A1 (https=) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2023370498B2 (en) * | 2022-10-28 | 2026-01-22 | Shanghai Deep Potential Technology Co., Ltd. | Aryl heterocyclic kv1.3 inhibitor, preparation method therefor, and use thereof |
| WO2024217515A1 (zh) | 2023-04-19 | 2024-10-24 | 上海复宏汉霖生物技术股份有限公司 | 一种杂环取代的芳香化合物、其制备方法及用途 |
| WO2025021167A1 (zh) * | 2023-07-26 | 2025-01-30 | 上海汇伦医药股份有限公司 | 芳基含氮杂环化合物、药物组合物和应用 |
| WO2025029769A1 (en) | 2023-07-31 | 2025-02-06 | Eli Lilly And Company | Solid forms of a kv1.3 potassium shaker channel blockers and method of using the same |
| WO2025235367A1 (en) * | 2024-05-06 | 2025-11-13 | D. E. Shaw Research, Llc | Azaindolinone compounds as kca3.1 potassium channel blockers |
| WO2025235362A1 (en) * | 2024-05-06 | 2025-11-13 | D. E. Shaw Research, Llc | INDOLINONE COMPOUNDS AS KCa3.1 POTASSIUM CHANNEL BLOCKERS |
Family Cites Families (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3854480A (en) | 1969-04-01 | 1974-12-17 | Alza Corp | Drug-delivery system |
| US4675189A (en) | 1980-11-18 | 1987-06-23 | Syntex (U.S.A.) Inc. | Microencapsulation of water soluble active polypeptides |
| US4452775A (en) | 1982-12-03 | 1984-06-05 | Syntex (U.S.A.) Inc. | Cholesterol matrix delivery system for sustained release of macromolecules |
| US5075109A (en) | 1986-10-24 | 1991-12-24 | Southern Research Institute | Method of potentiating an immune response |
| US5133974A (en) | 1989-05-05 | 1992-07-28 | Kv Pharmaceutical Company | Extended release pharmaceutical formulations |
| US5407686A (en) | 1991-11-27 | 1995-04-18 | Sidmak Laboratories, Inc. | Sustained release composition for oral administration of active ingredient |
| US5736152A (en) | 1995-10-27 | 1998-04-07 | Atrix Laboratories, Inc. | Non-polymeric sustained release delivery system |
| US6174908B1 (en) | 1999-05-10 | 2001-01-16 | Icagen, Inc. | Potassium channel inhibitors |
| GB0004297D0 (en) * | 2000-02-23 | 2000-04-12 | Ucb Sa | 2-oxo-1 pyrrolidine derivatives process for preparing them and their uses |
| US7495016B2 (en) * | 2002-10-21 | 2009-02-24 | Irm Llc | Pyrrolidones with anti-HIV activity |
| PT1805164E (pt) * | 2004-09-29 | 2011-04-11 | Sanofi Aventis | Derivados de 6-(piridinil)-4-pirimidona como inibidores de proteína-cinase tau 1 |
| MX2007008974A (es) * | 2005-01-28 | 2007-09-18 | Irm Llc | Sintesis de aril-pirrolidonas. |
| WO2011073273A1 (en) | 2009-12-16 | 2011-06-23 | Evotec Ag | Benzoxazine aryl sulfonamide derivatives as kv1.3 modulators |
| CN101979378B (zh) * | 2010-10-13 | 2012-06-27 | 中国科学院上海有机化学研究所 | 一种手性γ-内酰胺化合物的合成方法 |
| EP2655374B1 (en) * | 2010-12-20 | 2019-10-23 | Incyte Holdings Corporation | N-(1-(substituted-phenyl)ethyl)-9h-purin-6-amines as pi3k inhibitors |
| JP6599908B2 (ja) * | 2014-06-25 | 2019-10-30 | サンフォード−バーンハム メディカル リサーチ インスティテュート | ニューロテンシン受容体１の小分子アゴニスト |
| AU2020363356A1 (en) | 2019-10-07 | 2022-04-21 | D. E. Shaw Research, Llc | Arylmethylene heterocyclic compounds as Kv1.3 potassium shaker channel blockers |
| BR112022006292A2 (pt) | 2019-10-07 | 2022-06-28 | De Shaw Res Llc | Compostos heterobicílicos de arila como bloqueadores de canais de agitador de potássio kv1.3 |
| JP7822940B2 (ja) | 2019-10-07 | 2026-03-03 | ディー．イー．ショウ リサーチ，エルエルシー | Ｋｖ１．３カリウムシェーカーチャネル遮断薬としてのアリールメチレン複素環式化合物 |
| CN114728177B (zh) | 2019-10-07 | 2025-06-24 | D·E·萧尔研究有限责任公司 | 作为Kv1.3钾Shaker通道阻滞剂的芳基杂二环化合物 |
| MX2022004127A (es) | 2019-10-07 | 2022-06-14 | De Shaw Res Llc | Compuestos heterociclicos de arilo como bloqueadores del canal de potasio tipo shaker kv1.3. |
| CA3157026A1 (en) | 2019-10-07 | 2021-04-15 | D.E. Shaw Research, Llc | Arylmethylene aromatic compounds as kv1.3 potassium shaker channel blockers |
-
2021
- 2021-10-04 CN CN202180081847.5A patent/CN116782894A/zh active Pending
- 2021-10-04 MX MX2023003841A patent/MX2023003841A/es unknown
- 2021-10-04 EP EP21878284.5A patent/EP4225285A4/en active Pending
- 2021-10-04 CA CA3193554A patent/CA3193554A1/en active Pending
- 2021-10-04 WO PCT/US2021/053320 patent/WO2022076285A1/en not_active Ceased
- 2021-10-04 US US18/247,521 patent/US20230373952A1/en active Pending
- 2021-10-04 AU AU2021358700A patent/AU2021358700A1/en not_active Abandoned
- 2021-10-04 KR KR1020237015183A patent/KR20230082041A/ko not_active Withdrawn
- 2021-10-04 IL IL301627A patent/IL301627A/en unknown
- 2021-10-04 JP JP2023520423A patent/JP2023544404A/ja active Pending
- 2021-10-04 BR BR112023005387A patent/BR112023005387A2/pt not_active Application Discontinuation
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